Preparation and Characterization of TPGS‐Colloidal Silica Microparticles for Enhancement of Solubility and Oral Bioavailability of Lercanidipine Hydrochloride

Abstract

In this study, colloidal silica microparticles containing solubilizing excipient were prepared using the spray-drying process to enhance dissolution and oral absorption of lercanidipine hydrochloride. Several measurements including scanning electron microscopy, powder X-ray diffraction, particle size determination, in vitro dissolution, and pharmacokinetic study were conducted in rats. Among the tested solubilizing excipients, D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) dramatically enhanced the solubility of lercanidipine hydrochloride through micelle solubilization. In addition, TPGS-colloidal silica microparticles at the ratio of 1:10:10 (drug:TPGS:colloidal silica) showed rapid dissolution rate in all dissolution media and displayed higher area under the curve and maximum plasma concentration values compared with raw lercanidipine hydrochloride. Therefore, amorphous TPGS-colloidal silica microparticles fabricated using the spray-drying process have great potential in the clinical application of lercanidipine hydrochloride.

Improvement of Dissolution Rate of Oxcarbazepine Using Surface‐modified Solid Dispersion with Vinylpyrrolidone‐Vinyl Acetate Copolymer and Sucrose Laurate

“…Furthermore, dissolution efficiency (DE) was calculated according to the following equation: where y is the drug percent dissolved at time t . DE 120 was calculated by using the area under the dissolution profile at 120 min for the comparison of the surface‐modified solid dispersions . As shown in Table , the DE 120 values increased as the amount of PVP‐VA64 and sucrose laurate increased within the surface‐modified solid dispersion.…”

“…17,18 As shown in Table 2, the DE 120 values increased as the amount of PVP-VA64 and sucrose laurate increased within the surface-modified solid dispersion. 17,18 As shown in Table 2, the DE 120 values increased as the amount of PVP-VA64 and sucrose laurate increased within the surface-modified solid dispersion.…”

PLGA Nanoplatform for the Hypoxic Tumor Delivery: Folate Targeting, Therapy, and Ultrasound/Photoacoustic Imaging

“…22,23 D-α-tocopheryl polyethylene glycol 1000 succinate (Vitamin E TPGS or TPGS) is a new nonionic surfactant with amphipathic capabilities. 24,25 Its abilities to emulsify, disperse, gel, and solubilize poorly water-soluble medicines have been the subject of extensive research. 26 TPGS has been used to combat multidrug resistance and enhance the oral bioavailability of various anticancer medications.…”

Structural and Spectroscopic Characterization of TPGS Micelles: Disruptive Role of Cyclodextrins and Kinetic Pathways

“…TPGS has been extensively investigated for its solubilizing capacity in drug delivery [2][3][4] and approved by the FDA. Most studies in the literature have used TPGS-1000, which comprises 23 EO units, and a number of drug formulations based on this amphiphile have been developed, including micelles 5,6 , microparticles 7 , nanoparticles 8 and microemulsifying systems 9 , where TPGS is used as a solubilizer, absorption enhancer and a drug-carrier 10,11 , especially for poorly watersoluble drugs. Many of these studies have focused on the delivery of anticancer drugs 12 , since TPGS inhibits the activity of P-glycoproteins transporters (P-gp), which is responsible for the poor permeability of many cancer drugs through physiological barriers 13 .…”

“…The PEG chain bestows tocopherol with an amphiphilic character and self-aggregation capability, with the known advantages that nonionic amphiphiles have over cationic and anionic surfactants, in terms of their low sensitivity to electrolytes, good chemical stability, and generally better acceptability. TPGS has been approved by the Food and Drug Administration (FDA) and investigated for its solubilizing capacity in drug delivery. − Most studies in the literature have used TPGS-1000, which comprises 23 ethylene oxide (EO) units, and many drug formulations based on this amphiphile have been developed, including micelles, , microparticles, nanoparticles, and microemulsifying systems, where TPGS is used as an absorption enhancer and a drug carrier, , especially for poorly water-soluble drugs. Some of these studies have focused on the delivery of anticancer drugs because TPGS inhibits the activity of P-glycoprotein transporters (P-gp), which is responsible for the poor permeability of many cancer drugs through physiological barriers .…”